51st week of 2013 patent applcation highlights part 51 |
Patent application number | Title | Published |
20130338098 | Topical Analgesic Compositions Containing Aliphatic Polyamines and Methods of Using Same - A method for producing local analgesia in a subject having a site of local discomfort comprises administration of an aliphatic polyamine and, preferably, urea. A composition of the invention comprises an aliphatic polyamine and preferably urea. The polyamine can be an alkylamine, such as, preferably, putrescine. The composition can also include lidocaine and/or a copper containing component. | 2013-12-19 |
20130338099 | MERCAPTO-MODIFIED BIOCOMPATIBLE MACROMOLECULE DERIVATIVES WITH LOW DEGREE OF MERCAPTO-MODIFICATION AND THE CROSS-LINKED MATERIALS AND USES THEREOF - The present invention discloses a mercapto-modified biocompatible macromolecule derivative with a low degree of modification. The mercapto-modified biocompatible macromolecule derivative not only maintains the initial structure, physiological function and biocompatibility as much as possible, but also allows the preparation of the biocompatible macromolecule cross-linked material with a low degree of cross-linking through the effectively chemical cross-linking with the introduced mercapto group. The present invention further discloses a disulfide-bond cross-linked biocompatible macromolecule material with a very low degree of cross-linking. The disulfide-bond cross-linked biocompatible macromolecule material not only maintains the initial structure, physiological function and biocompatibility of the biocompatible macromolecule as much as possible, but also effectively prolongs turn over and reduces the solubility of the biocompatible macromolecule in vivo, better meeting the requirements of various clinical applications. The present invention further relates to the application of the disulfide-bond cross-linked biocompatible macromolecule material in the field of medicine and pharmacy. | 2013-12-19 |
20130338100 | Method of Cross-Linking Hyaluronic Acid with Divinylsulfone - The present invention relates to methods of producing a homogenous hydrogel comprising hyaluronic acid, or salt thereof, crosslinked with divinylsulfone (DVS), said method comprising the steps of (a) providing an alkaline solution of hyaluronic acid, or salt thereof; (b) adding DVS to the solution of step (a), whereby the hyaluronic acid, or salt thereof, is crosslinked with the DVS to form a gel; (c) treating the gel of step (b) with a buffer, wherein the gel swells and forms a hydrogel comprising hyaluronic acid, or salt thereof, crosslinked with DVS. | 2013-12-19 |
20130338101 | CELL-ADHESIVE, ENZYMATICALLY CROSSLINKED FLAVONOID HYDROGELS AND METHODS FOR MAKING SAME - There are provided methods for producing a hydrogel that is capable of adhesion of cells and which comprises enzymatically cross-linked conjugates of a hydrogel forming agent and a flavonoid, formed from a reaction using peroxide and peroxidase. Hydrogels produced by such methods and methods of using the hydrogels are also provided. | 2013-12-19 |
20130338102 | METHODS AND COMPOSITIONS FOR DETECTION OF MICROBIAL CONTAMINANTS IN PERITONEAL DIALYSIS SOLUTIONS - Methods and compositions for detection of microbial contaminants in peritoneal dialysis solutions are provided. A novel cause of aseptic peritonitis is provided—aseptic peritonitis associated with gram positive microbial contamination of a dialysis solution. Peptidoglycan is a major component of a gram positive bacterial cell wall and thus can serve as a marker for gram positive bacteria. In this regard, testing for peptidoglycans can be utilized to effectively prevent peritonitis in patients that use the peritoneal dialysis solutions, such as peritoneal dialysis solutions that contain a glucose polymer including an icodextrin and the like. | 2013-12-19 |
20130338103 | TREATMENT OF CANCER - Provided are methods relating to compositions that include a CDP-topoisomerase inhibitor, e.g., a CDP-camptothecin or camptothecin derivative conjugate, e.g., CRLX101. | 2013-12-19 |
20130338104 | 3-Substituted-4-Oxo-3,4-Dihydro-Imidazo[5,1-d]1,2,3,5-Tetrazine-8-Carboxyl- ic Acid Amides and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds. | 2013-12-19 |
20130338105 | IMINIPYRIDINE DERIVATIVES AND THEIR USES AS MICROBIOCIDES - Compounds of the formula I | 2013-12-19 |
20130338106 | COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY - Disclosed are compounds of Formula I: and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO | 2013-12-19 |
20130338107 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Provided herein are compounds of formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof or mixtures thereof, wherein Z | 2013-12-19 |
20130338108 | PHENYL BICYCLIC METHYL AMINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel phenyl bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2013-12-19 |
20130338109 | SUBSTITUTED BICYCLIC METHYL AMINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 2013-12-19 |
20130338110 | MITOCHONDRIA TARGETED CATIONIC ANTI-OXIDANT COMPOUNDS FOR PREVENTION, THERAPY OR TREATMENT OF HYPER-PROLIFERATIVE DISEASE, NEOPLASIAS AND CANCERS - The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups. | 2013-12-19 |
20130338111 | Sulfonamide Derivatives - The present invention relates to compounds of the formula | 2013-12-19 |
20130338112 | COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention relates to compounds of structural formula (I): | 2013-12-19 |
20130338113 | MATERIALS AND METHODS FOR TREATING VIRAL INFECTIONS - The subject invention provides materials and methods for treating various health conditions, including the prevention and/or treatment of a viral infection. In a preferred embodiment, a cysteamine compound is administered to a subject to treat an influenza virus infection. More preferably, a cysteamine compound is administered to a subject to treat influenza A, influenza B, influenza C virus infections, including avian influenza virus subtypes (such as H5N1 avian influenza virus). | 2013-12-19 |
20130338114 | COMPOSITIONS FOR INCREASING STRENGTH, MUSCLE MASS, AND LEAN BODY MASS - Phosphatidic acid, lyso-phosphatidic acid, and/or phospholipase D can be administered to exercising mammals to increase muscle mass and strength. These actives can be administered orally to aging, bedridden or cachectic patients, as well as resistance training individuals, to improve nitrogen balance. The oral administration of phosphatidic acid as well as other actives described herein was found to increase muscle hypertrophy, strength, and lean body mass, and to decrease body fat in subjects, for example, when combined with resistance training. | 2013-12-19 |
20130338115 | USE OF MITOCHONDRIALLY-ADDRESSED COMPOUNDS FOR PREVENTING AND TREATING CARDIOVASCULAR DISEASES - The invention relates to pharmacology and medicine, in particular to a class of mitochondrially-addressed compounds which can be used in the pharmaceutical compositions of medicinal agents (preparations) for preventing and treating cardiovascular diseases and diseases and pathological conditions caused by disturbed blood circulation or oxygen supply to tissues and organs. | 2013-12-19 |
20130338116 | COMPOUNDS AND METHODS FOR THE TREATMENT OF PAIN AND OTHER DISEASES - The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound. | 2013-12-19 |
20130338117 | THERAPEUTIC COMPOUNDS FOR BLOCKING DNA SYNTHESIS OF POX VIRUSES - This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided. | 2013-12-19 |
20130338118 | COMPOUNDS FOR TREATMENT OF HEART FAILURE - A combination of: a first tetracycline (TC) component; and a second component capable of releasing nitric oxide (NO) or a nitrate capable of mimicking NO effects in vivo (NO mimetic). The combinations of the invention advantageously act as more effective MMP modulators with selective reductions in circulating MMP-9 levels in-vivo and inhibitory effects on MMP-2 and MMP-9 levels in-vitro. The combinations of the invention also advantageously act as modulators of inflammation mediators. The co-existence of abnormalities of MMP enzymes and inflammation in many diseases make these characteristics advantageous. Therefore, the various combinations of the invention find utility in medical applications where MMPs and/or inflammation is implicated. | 2013-12-19 |
20130338119 | Pyrrolidinone Benzenesulfonamide Derivatives as Modulators of Ion Channels - The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 2013-12-19 |
20130338120 | Aspirin Derivatives and Uses Thereof - The present invention provides novel aspirin derivatives useful for preventing and/or treating cancer. The novel compounds of this invention may be particularly useful for the prevention and/or treatment of cancers affecting the gastrointestinal system, such as colorectal cancer. | 2013-12-19 |
20130338121 | TWO SPEED MONOLITHIC SYSTEM FOR CONTROLLED RELEASE OF DRUGS - The present document describes a monolithic tablet dosage form for delivery of an active ingredient at two different release rates comprising a carboxyl polymer complexed with a multivalent cation and a disintegrating agent for a first initial fast release of the active ingredient, and a modulating agent for a second sustained release of the active ingredient. Also described are processes for preparing the carboxyl polymer complexed with a multivalent cation, and carboxyl polymer made from the process. | 2013-12-19 |
20130338122 | TRANSDERMAL HORMONE REPLACEMENT THERAPIES - Hormone replacement therapies are provided comprising solubilized progesterone alone and optionally with an estrogen, cyclic/sequential and continuous-combined dosing, and administered via transdermal HRT delivery systems. | 2013-12-19 |
20130338123 | NATURAL COMBINATION HORMONE REPLACEMENT FORMULATIONS AND THERAPIES - Estrogen and progesterone replacement therapies are provided herein. Among others, the following formulations are provided herein: solubilized estradiol without progesterone; micronized progesterone without estradiol; micronized progesterone with partially solubilized progesterone; solubilized estradiol with micronized progesterone; solubilized estradiol with micronized progesterone in combination with partially solubilized progesterone; and solubilized estradiol with solubilized progesterone. | 2013-12-19 |
20130338124 | ORGANIC COMPOUNDS - The present invention relates to (1- or 2- and/or 5 and/or 7-substituted)-(3-oxy)-(4H, 4-imino, 4-thioxo or 4-oxo)-pyrazolo[3,4-d]pyrimidin-6-ones, e.g., a compound of formula II as described below, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them. Of particular interest are novel compounds useful as inhibitors of phosphodiesterase 1 (PDE1), e.g., in the treatment of diseases involving disorders of the dopamine D1 receptor intracellular pathway, such as Parkinson's disease, depression, narcolepsy, damage to cognitive function, e.g., in schizophrenia, or disorders that may be ameliorated through enhanced progesterone-signaling pathway, e.g., female sexual dysfunction. | 2013-12-19 |
20130338125 | TREATMENT METHODS USING PHARMACEUTICAL SOLID STATE FORMS - The invention provides and describes solid state 17α-ethynyl-5α-androstane-3α,17β-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-5α-androstane-3α,17β-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17α-ethynyl-5α-androstane-3α,17β-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-5α-androstane-3α,17β-diol and uses of such formulations in treating the described conditions. | 2013-12-19 |
20130338126 | Ophthalmic Suspension for Ocular Use - A gatifloxacin and prednisolone topical ophthalmic pharmaceutical compositions for prevention and treatment of ophthalmic bacterial infections and inflammatory conditions associated with pre-surgical and/or post surgical ocular surgeries. | 2013-12-19 |
20130338127 | TRIAMCINOLONE ACETONIDE FORMULATIONS FOR TREATING DERMATITIS AND PSORIASIS - The present invention is drawn to formulations and related methods for treating dermatitis or psoriasis. The formulation can include triamcinolone acetonide, a polymer selected from the group of a poly(2-hydroxyalkylacrylate), a poly(2-hydroxyalkylmethacrylate), and combinations thereof. The formulation also includes a volatile solvent system including at least one volatile solvent, and a non-volatile solvent system including at least one non-volatile solvent. | 2013-12-19 |
20130338128 | PLATINUM-N-HETEROCYCLIC CARBENE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to the platinum N-heterocycle derivatives of general formula (I) | 2013-12-19 |
20130338129 | METHOD OF TREATING REFRACTORY CANCER - Therapeutic methods for treating refractory cancers are disclosed comprising administering to a patient in need of treatment a ruthenium complex salt. | 2013-12-19 |
20130338130 | METHYLSULFONYLMETHANE (MSM) FOR TREATMENT OF DRUG RESISTANT MICROORGANISMS - Embodiments of the invention relate generally to the use of compositions comprising methylsulfonylmethane (MSM), and one or more therapeutic agents, for the treatment of drug-sensitive and drug resistant microorganisms. In several embodiments, such compositions are effective in treating drug resistant infectious diseases, for example, MRSA. | 2013-12-19 |
20130338131 | PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION COMPRISING A LOW SOLUBLE PHARMACEUTICALLY ACTIVE INGREDIENT - The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing a pharmaceutical composition comprising a pharmaceutically active ingredient (API) that is poorly soluble in water, a pharmaceutical composition obtained according to said process, to a dosage form comprising said pharmaceutical composition and to the use of said dosage forms for the treatment of hypercholesterolemia. | 2013-12-19 |
20130338132 | HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE - Compounds represented by the following formula (I), | 2013-12-19 |
20130338133 | SUBSTITUTED IMIDAZOPYRIDAZINES - The present invention relates to substituted imidazopyridazine compounds of general formula (I), which are Mps-1 (Monopolar Spindle 1) Kinase inhibitors (also known as Tyrosine Threonine Kinase, TTK) in which R | 2013-12-19 |
20130338134 | SUBSTITUTED TRICYCLIC COMPOUNDS AS FGFR INHIBITORS - The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. | 2013-12-19 |
20130338135 | PHENYL BICYCLIC METHYL AZETIDINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel phenyl bicyclic methyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2013-12-19 |
20130338136 | NOVEL INDOLE MODULATORS OF S1P RECEPTORS - The present invention relates to novel indole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2013-12-19 |
20130338137 | Substituted annellated pyrimidines and use thereof - The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases. | 2013-12-19 |
20130338138 | AZETIDINE AND PIPERIDINE COMPOUNDS USEFUL AS PDE10 INHIBITORS - Azetidine and piperidine compounds of formula (I): | 2013-12-19 |
20130338139 | THERAPEUTIC THIOPHENE-, FURAN-, AND PYRIDINE-FUSED AZOLOPYRIMIDIN-5-(6H)-ONES - Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders. | 2013-12-19 |
20130338140 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I wherein Z, Z | 2013-12-19 |
20130338141 | HIV INTEGRASE INHIBITORS - Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: | 2013-12-19 |
20130338142 | IMIDAZOPYRAZINE SYK INHIBITORS - Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided. | 2013-12-19 |
20130338143 | Compositions for Transdermal Delivery of Active Agents - Disclosed herein are compositions that are useful in effecting the transdermal delivery of therapeutic agents. More particularly, the disclosed transdermal compositions may include a fatty alcohol (for example, octanol), a terpene (for example, limonene), and an active agent comprising an amine moiety. | 2013-12-19 |
20130338144 | uPAR-uPA INTERACTION INHIBITORS AND METHODS FOR TREATING CANCER - The invention described herein pertains to compounds, compositions and formulations comprising the compounds, and methods for use of the compounds, compositions and/or formulations in the treatment of diseases responsive to the inhibition of uPAR-uPA interactions, such as cancer. | 2013-12-19 |
20130338145 | Method for Mediating Dopamine Receptor-Driven Reacidification of Lysosomal pH - Provided is a method of treating or preventing age-related macular degeneration (AMD) or Stargardt's disease in a patient subject to, or symptomatic of the disease, whereby normal lysosomal pH (pH | 2013-12-19 |
20130338146 | MULTIFUNCTIONAL NITROXIDE DERIVATIVES AND USES THEREOF - Multifunctional nitroxide derivatives comprising a potassium channel opener and a reactive oxygen species (ROS) degradation catalyst that can act as an anti-oxidant, as well as pharmaceutical compositions comprising them are provided. The multifunctional compounds and pharmaceutical compositions are useful for treatment of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction. | 2013-12-19 |
20130338147 | 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES - The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. | 2013-12-19 |
20130338148 | PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. | 2013-12-19 |
20130338149 | SEDATIVE FOR USE DURING EYE SURGERY - A drug for sedating a patient, and especially a smoker, during eye surgery. The drug includes a sedative such as midazolam in a mix with nicotine. The mixture is injected into the patient prior to the eye surgery. | 2013-12-19 |
20130338150 | DI AND TRI - SUBSTITUTED OXATHIAZINE DERIVATIVES, METHOD FOR THE PRODUCTION, METHOD FOR THE PRODUCTION THEREOF, USE THEREOF AS MEDICINE AND DRUG CONTAINING SAID DERIVATIVES AND USE THEREOF - The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia. | 2013-12-19 |
20130338151 | FUSED RING ANALOGUES OF ANTI-FIBROTIC AGENTS - The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders. | 2013-12-19 |
20130338152 | FLUOROPHENYL BICYCLIC HETEROARYL COMPOUNDS - The present invention provides a compound the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 2013-12-19 |
20130338153 | 8-(2'-HETEROCYCYL)PYRIDO[2.3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders. | 2013-12-19 |
20130338154 | MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Pyrrole compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. | 2013-12-19 |
20130338155 | METHOD FOR TREATING INFECTIONS - The present invention relates to compounds that inhibit the activity of Hsp90 and methods of using these compounds for treating or preventing infection. | 2013-12-19 |
20130338156 | IMIDAZOPYRIDIN-2-ONE DERIVATIVES - A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof. | 2013-12-19 |
20130338157 | AZAINDAZOLE COMPOUNDS AND METHODS OF USE - Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists. | 2013-12-19 |
20130338158 | 6-SUBSTITUTED INDOLE-3-CARBOXYLIC ACID AMIDE COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ANTAGONIST BIOLOGICAL ACTIVITY - The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: | 2013-12-19 |
20130338159 | BI-HETEROARYL COMPOUNDS AS VPS34 INHIBITORS - The present invention includes novel methods of treating a disease or disorder characterized by hyperactivity of Vps34, and compound as Vps34 inhibitors; particularly compounds of Formula I or a pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Vps34 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof. | 2013-12-19 |
20130338160 | Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-d- ione structural scaffold, their biological activity, and uses thereof - The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof. | 2013-12-19 |
20130338161 | AXL INHIBITORS FOR USE IN COMBINATION THERAPY FOR PREVENTING, TREATING OR MANAGING METASTATIC CANCER - This invention is directed to methods of preventing, treating or managing cancer, preferably metastatic cancer, in a patient. The methods comprise administering an effective amount of an Axl inhibitor in combination with the administration of an effective amount of one or more chemotherapeutic agents. | 2013-12-19 |
20130338162 | COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS - Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. | 2013-12-19 |
20130338163 | VINYL-ARYL DERIVATIVES FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders. | 2013-12-19 |
20130338164 | Multimeric VLA-4 Antagonists Comprising Polymers Moieties - Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis. | 2013-12-19 |
20130338165 | Use of Compounds Elevating Glutathione Levels for the Treatment of Parkinson's Disease - Methods of treating Parkinson's Disease comprising administering compounds that up-regulate cystine-glutamate exchange (system X | 2013-12-19 |
20130338166 | REDUCING SIDE EFFECTS OF TRAMADOL - The invention provides methods of reducing the side effects of tramadol. Accordingly, in one embodiment, the invention provides a method of reducing the incidence of newly-discovered side effects related to sexual function in human males taking a tramadol material. The method comprises administering a phosphodiesterase inhibitor to a male taking the tramadol material. The invention also provides pharmaceutical compositions. In one embodiment, the composition comprises a tramadol material and a phosphodiesterase inhibitor. The invention further provides kits. In one embodiment, the kit comprises a tramadol material and a phosphodiesterase inhibitor. | 2013-12-19 |
20130338167 | TARTRATE SALTS OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives of Formula II, below: | 2013-12-19 |
20130338168 | Combinations of JAK Inhibitors - The invention provides a pharmaceutical combination comprising:
| 2013-12-19 |
20130338169 | METHODS OF USE OF INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME - The present invention relates to inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids. | 2013-12-19 |
20130338170 | TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF - The invention relates to compounds of formula IA | 2013-12-19 |
20130338171 | Pharmaceutically Acceptable Salts of Quinolinone Compounds Having Improved Pharmaceutical Properties - A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R | 2013-12-19 |
20130338172 | CRYSTALLINE FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR - Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2013-12-19 |
20130338173 | Carbocycle-Substituted Purine And 7-Deazapurine Compounds - The present invention relates to carbocycle-substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 2013-12-19 |
20130338174 | PURINE DERIVATIVES - The invention provides the compound of formula (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy. | 2013-12-19 |
20130338175 | Multi-Arm Polymeric Prodrug Conjugates of Pemetrexed-Based Compounds - Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the pemetrexed-based compound is achieved. | 2013-12-19 |
20130338176 | METHODS OF PREVENTING AND TREATING HYPERLIPIDEMIA OR ATHEROSCLEROSIS - The present invention provides methods and therapeutic agents for lowering serum or plasma serotonin levels in a patient in order to prevent or treat hyperlipidemia or atherosclerosis. In preferred embodiments, the patient is known to have, or to be at risk for, hyperlipidemia or atherosclerosis and the agents are TPH1 inhibitors. | 2013-12-19 |
20130338177 | Spiro-Amino-Imidazolone and Spiro-Amino-Dihydro-Pyrimidinone Compounds as Beta-Secretase Modulators and Methods of Use - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I), wherein variables A | 2013-12-19 |
20130338178 | SIRTUIN MODULATORS AS INHIBITORS OF CYTOMEGALOVIRUS - Agents and methods of inhibiting or improving the growth of viruses are provided. | 2013-12-19 |
20130338179 | DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT | 2013-12-19 |
20130338180 | FORMULATION COMPRISING PHENYLAMINOPYRIMIDINE DERIVATIVE AS ACTIVE AGENT - An oral pharmaceutical formulation containing an effective amount of NRC-AN-019 including its pharmaceutically acceptable salts and polymorphs such as Form I, Form II and Form III thereof to improve the bioavailability intended for self-emulsification upon its contact with the gastro-intestinal fluid. The invention also relates to a process for the preparation of oral solution containing NRC-AN-019 in an effective concentration for the better therapy against Chronic Myeloid Leukemia as BCR-ABL tyrosine kinase inhibitor and against other tumors such as head and neck cancer, prostate cancer and the like. | 2013-12-19 |
20130338181 | TREATMENT OF EFFECT OF CHEMICALS WITH THEIR ULTRADILUTE STEREOISOMERS - A method of treating an effect of a chemical agent, which agent is characterized by one or more chiral centres, by administering a dilution or an ultra-high dilution or potentised preparation of a stereoisomer of said chemical agent. | 2013-12-19 |
20130338182 | NOVEL MORPHINANS USEFUL AS ANALGESICS - Compounds of Formula (I) are disclosed. | 2013-12-19 |
20130338183 | COMPOSITIONS AND METHODS FOR MOBILIZING STEM CELLS - The present invention relates to the field of hematopoietic stem cells. More specifically, the present invention provides methods and composition useful for peripheral blood stem cell mobilization. In one embodiment, a method of treating an organ transplant recipient comprises administering to the recipient a low dose of Tacrolimus in an amount sufficient to mobilize stem cells to the peripheral blood of the recipient. In a specific embodiment, the low dose of Tacrolimus is in the range of about 0.05 mg/kg to about 0.5 mg/kg. | 2013-12-19 |
20130338184 | 2-AMINO-NAPHTHYRIDINE DERIVATIVES - The invention in one embodiment is directed to a compound of Formula A: | 2013-12-19 |
20130338185 | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) | 2013-12-19 |
20130338186 | AMIDES OF ACETIC AND PROPIONIC ACIDS - The invention relates to novel amides of acetic and propionic acids, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning ability and memory. | 2013-12-19 |
20130338187 | Novel 1-(1-OXO-1,2,3,4-TETRAHYDROISOQUINOLIN-7-YL)Urea Derivatives As N-FORMYL Peptide Receptor Like-1 (FPRL-1) Receptor Modulators - The present invention relates to novel 1-(1-Oxo-1,2,3,4-tetrahydroisoquinolin-7-yl)urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. | 2013-12-19 |
20130338188 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 2013-12-19 |
20130338189 | CRYSTAL OF ANTI-BACTERIAL COMPOUND - It is intended to provide a salt of a compound and crystals thereof useful as a therapeutic and/or preventive agent for infectious diseases which has wide and excellent antibacterial activity and has excellent safety. | 2013-12-19 |
20130338190 | PHARMACEUTICALLY ACCEPTABLE SALT OF (E)-N-[4-[[3-CHLORO-4-(2-PYRIDYLMETHOXY)PHENYL]AMINO]-3-CYANO-7-ETHOXY-6-- QUINOLYL]-3-[(2R)-1-METHYLPYRROLIDIN-2-YL]PROP-2-ENAMIDE, PREPARATION METHOD THEREOF, AND MEDICAL USE THEREOF - Provided as represented by formula (I) is a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide, a preparation method thereof, and a use thereof as a therapeutic agent, and especially as a protein kinase inhibitor. | 2013-12-19 |
20130338191 | CRYSTALLINE FREEBASE FORMS OF A BIPHENYL COMPOUND - The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder. | 2013-12-19 |
20130338192 | METHOD FOR AUGMENTING THE EFFECTS OF SEROTONIN REUPTAKE INHIBITORS - A method of treating a subject for a serotonergic neurotransmission dysregulation disorder, comprises administering the subject a serotonin enhancer (e.g., a serotonin reuptake inhibitor) in an amount effective to treat the disorder; and concurrently administering the subject 5-hydroxytryptophan in an amount effective to enhance the activity of the serotonin enhancer, (e.g., serotonin reuptake inhibitor). In preferred embodiments the disorder is depression, anxiety, or substance abuse. | 2013-12-19 |
20130338193 | CHIRAL 1-(4-METHYLPHENYLMETHYL)-5-OXO--PYRROLIDINE-2-CARBOXAMIDES AS INHIBITORS OF COLLAGEN INDUCED PLATELET ACTIVATION AND ADHESION - Chiral 1-(4-methylphenylmethyl)-5-oxo-{N-[(3-t-butoxycarbonyl-aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion The present invention provides chiral (2S)-1-(4-methyl-phenylmethyl)-5-oxo-(3S)-{N-[(3-t butoxycarbonyl aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide, and (2S)-1-(4-methylphenylmethyl)-5-oxo-(3R)-{N-[(3-t-butoxycarbonyl amino methyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide of formula 6 and 7 respectively. The present invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors. The present invention provides a process for preparation of chiral carboxamides of formula 6 and 7 using the process which has advantage to avoid any racemization at the a-carboxylic center, during N-alkylation. The reagent LiHMDS is used at low temperatures to furnish methyl N-(p methylphenylmethyl)lpyroglutamate in good chiral purity. | 2013-12-19 |
20130338194 | Predicting Atrial Fibrillation Recurrence by Protease and Protease Inhibitor Profiling - Disclosed herein are methods of and systems for predicting recurrence of atrial fibrillation comprising protease and protease inhibitor profiling. | 2013-12-19 |
20130338195 | NOVEL PYRIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2013-12-19 |
20130338196 | ALPHA-KETOHETEROCYCLES AND METHODS OF MAKING AND USING - Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones. | 2013-12-19 |
20130338197 | PARASITE- AND HYGIENIC PEST-CONTROLLING AGENT - There is provided a novel agent for controlling harmful arthropods or nematodes that are parasites and hygienic pests for animals. An ecto- or endo-parasiticide for mammals or the like comprising as active ingredient, one or more selected from substituted benzamide compounds of formula (1) or salts thereof: | 2013-12-19 |